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Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

"Protecting neurons from death during oxidative and neuroexcitotoxic stress is key for preventing cognitive dysfunction. We uncovered a novel neuroprotective mechanism involving interaction between neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor with no previously known neurological function. Co-immunoprecipitation and pull-down assays confirmed interaction between NFα1/CPE and 5-HTR1E and 125I NF-α1/CPE-binding studies demonstrated saturable, high-affinity binding to 5-HTR1E in stably transfected HEK293 cells (Kd = 13.82 nM). Treatment of 5-HTR1E stable cells with NF-α1/CPE increased pERK 1/2 and pCREB levels which prevented a decrease in pro-survival protein, BCL2, during H2O2-induced oxidative stress. Cell survival assay in β-arrestin Knockout HEK293 cells showed that the NF-α1/CPE-5-HTR1E-mediated protection against oxidative stress was β-arrestin-dependent. Molecular dynamics studies revealed that NF-α1/CPE interacts with 5-HTR1E via 3 salt bridges, stabilized by several hydrogen bonds, independent of the serotonin pocket. Furthermore, after phosphorylating the C-terminal tail and intracellular loop 3 (ICL3) of NF-α1/CPE-5-HTR1E, it recruited β-arrestin1 by forming numerous salt bridges and hydrogen bonds to ICL2 and ICL3, leading to activation of β-arrestin1. Immunofluorescence studies showed 5-HTR1E and NF-α1/CPE are highly expressed and co-localized on cell surface of human hippocampal neurons. Importantly, knock-down of 5-HTR1E in human primary neurons diminished the NF-α1/CPE-mediated protection of these neurons against oxidative stress and glutamate neurotoxicity-induced cell death. Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB/BCL2 pathway to mediate stress-induced neuroprotection." Read full article

partnerships and collaborations across pharma and #biotech⁠ and is an advocate for the role of #AI in drug discovery." Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

chemistry decisions Why Live-cell High-Content Screening Matters for CB2 Ligand Profiling CB2 is a GPCR For GPCR programs—where trafficking, receptor reserve, and internalization are common confounders—access What This Means for CB2 Drug Discovery Programs Taken together, the dataset offers several insights into how live-cell HCS can support CB2 ligand discovery: 1. For researchers working in cannabinoid pharmacology, inflammation, or GPCR-mediated analgesia, these

We have achieved a great deal in the last decade, such as the first-ever AI-designed drug candidates We’re excited about delivering the next ten years of Exscientia and advancing AI to design better drugs #artificialintelligence #drugdesign #drugdiscovery" Read more at the source #DrGPCR #GPCR #IndustryNews

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while In this way, we present the analysis of a series of GPCRs whose activity has been shown to affect the Our compilation of data revealed that the mechanisms most involved in the role of GPCRs in lifespan are We also discuss the possibility of using agonist or antagonist drugs, depending on the beneficial or harmful effects of each GPCR, in order to prolong people's lifespan and healthspan.

allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors (GPCRs To chemically induce CCR9 degradation, we then developed the first PROTAC targeting the IABS of GPCRs our CCR9-PROTAC is able to reduce CCR9 levels, thereby offering an unprecedented approach to modulate GPCR

protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs their secretion of insulin, and islet function can be modified by ligands acting at the large number of GPCRs is altered under pathophysiological conditions and, in this review, we have compared expression of GPCR We have also considered the likely outcomes on islet function that the altered GPCR expression status confers and the possible impact that adipokines, secreted from expanded fat depots, could have at those GPCRs

Watch Episode 168 In drug discovery, tools matter, but so do people. In Episode 168 of the Dr. GPCR so powerful. “We don’t just deliver compounds, we solve assay problems.” — Dr. . 👉 See how Celtarys can support your drug discovery workflow on the company page . _______________ Keyword Cloud:   GPCR data platform , fluorescent ligands , assay development , GPCR research community GPCR ecosystem , GPCR webinar series

revisit core pharmacology concepts, master new ones, and sharpen your thinking to directly advance your drug discovery program.   GPCR Ecosystem, we're giving Dr. Just the thinking and tools drug discovery demands. GPCR Team & Terry’s Desk

At Alkermes , Sokhom Pin wasn’t just leading GPCR programs; he was building culture from the ground up Why Culture Matters in Drug Discovery You can’t innovate under pressure. In a field like GPCR research (where data complexity and failure rates are high), scientific rigor thrives From Lab Bench to Boardroom His work at Alkermes didn’t just improve drug screening outcomes, it redefined GPCR ecosystem , GPCR research community , GPCR podcast , GPCR data platform , GPCR training program

Welcome Back, Discovery Drivers   Terry’s Corner is live, on-demand pharmacology built for drug discovery Elevate your drug discovery program with 45+ lessons yearly. Read The Full Article GPCR Publication Highlights   Chemokine–GPCR Selectivity Unveiled Sequence- and NMBR, with allosteric communication hubs modulating signaling, advancing antipruritic drug strategies GPCR Team Join Our Newsletter!

vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors (GPCRs This review discusses the signalling mechanisms of GHSR1a alone and in combination with other GPCRs, and explores the physiological consequences of GHSR1a coupling with other GPCRs.

of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled receptors (GPCRs Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed expressed in mast cells, macrophages, and in cardiovascular tissue, linking them to pseudo-allergic drug mediator and supports the notion that IL-6 can be used as a marker for MRGPRD activation in an in vitro drug

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs Using current knowledge on class A GPCRs and existing experimental data in the literature as constraints

Her work in the field has been instrumental and is set to shape the future of drug discovery for years #DrugDiscovery #MassSpec #Award #massspectrometry" Read more at the source #DrGPCR #GPCR #IndustryNews

receptor-ligand complexes: Impact of ligand type and receptor activation state G protein-coupled receptors (GPCR Their abundance and role in nearly all physiological systems make GPCR the largest protein family targeted Ligand discovery aimed at identification of chemical tools and drug leads is aided by molecular docking provided broadly generalizable performance expectations for docking into experimentally-characterized GPCR Simulations were performed using 37 experimental structures of 11 Class A GPCR crystallized in multiple

pulmonary fibrosis, cancers, cardiovascular diseases and neuropathic pain, making it a promising target for drug While no drugs targeting LPARs have been approved by the FDA thus far, at least three antagonists have

#ForbesUnder30 #ArcoScreen #sciences #EPFL" Read more at the source #DrGPCR #GPCR #IndustryNews

Read more at the source #DrGPCR #GPCR #IndustryNews

structural positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling may not be enriched within a single gene but rather that cognate mutations with similar effects on GPCR To test this possibility, we systematically aggregated somatic cancer mutations across class A GPCRs The possibility that multiple different GPCRs could moonlight as drivers or enablers of a given cancer

Hello GPCR Innovators ,   We’re preparing to launch Terry’s Corner, a new knowledge hub shaped by Dr. Terry Kenakin’s decades of GPCR insight. Meanwhile, incretin and amylin-based therapies are reshaping the obesity drug landscape. It’s a story of leadership, scientific rigor, and tools built for the needs of modern discovery teams GPCR Team

mechanosensation-dependent behavior in C. elegans via a trans function Latrophilins are highly conserved Adhesion GPCRs